School of Chemistry, Sun Yat-Sen University, Guangzhou 510275, China.
MOE Key Laboratory of Bioinorganic and Synthetic Chemistry, Sun Yat-Sen University, Guangzhou 510275, China.
Molecules. 2022 Apr 10;27(8):2439. doi: 10.3390/molecules27082439.
Quorum sensing (QS) is a cell-to-cell communication process that controls bacterial collective behaviors. The QS network regulates and coordinates bacterial virulence factor expression, antibiotic resistance and biofilm formation. Therefore, inhibition of the QS system is an effective strategy to suppress the bacterial virulence. Herein, we identify a phosphate ester derivative of chrysin as a potent QS inhibitor of the human pathogen () using a designed luciferase reporter assay. In vitro biochemical analysis shows that the chrysin derivative binds to the bacterial QS regulator LasR and abrogates its DNA-binding capability. In particular, the derivative exhibits higher anti-virulence activity compared to the parent molecule. All the results reveal the potential application of flavone derivative as an anti-virulence compound to combat the infectious diseases caused by .
群体感应（QS）是一种细胞间通讯过程，控制着细菌的集体行为。QS 网络调节和协调细菌毒力因子的表达、抗生素耐药性和生物膜形成。因此，抑制 QS 系统是抑制细菌毒力的有效策略。在这里，我们使用设计的荧光素酶报告基因检测法，鉴定出一种紫檀芪的磷酸酯衍生物，它是人类病原体 （）的一种有效的 QS 抑制剂。体外生化分析表明，紫檀芪衍生物与细菌 QS 调节剂 LasR 结合，并使其 DNA 结合能力丧失。特别是，该衍生物表现出比母体分子更高的抗毒力活性。所有结果表明，类黄酮衍生物作为一种抗毒力化合物，具有潜在的应用价值，可以用于防治由 引起的传染病。
